Propecia Research Today is a free monthly online journal that collates and summarizes the latest research about Propecia, including details on baldness, hair loss, side-effects, results.

New 5alpha-reductase inhibitors: in vitro and in vivo effects.

Pérez-Ornelas V, Cabeza M, Bratoeff E, Heuze I, Sánchez M, Ramírez E, Naranjo-Rodríguez E

Department of Pharmacy, Faculty of Chemistry, National University of Mexico City, Mexico D.F., Mexico.

The enzyme 5alpha-reductase is responsible for the conversion of testosterone (T) to its more potent androgen dihydrotestosterone (DHT). This steroid had been implicated in androgen-dependent diseases such as: benign prostatic hyperplasia, prostate cancer, acne and androgenic alopecia. The inhibition of 5alpha-reductase enzyme offers a potentially useful treatment for these diseases. In this study, we report the synthesis and pharmacological evaluation of several new 3-substituted pregna-4, 16-diene-6, 20-dione derivatives. These compounds were prepared from the commercially available 16-dehydropregnenolone acetate. The biological activity of the new steroidal derivatives was determined in vivo as well as in vitro experiments. In vivo experiments, the anti-androgenic effect of the steroids was demonstrated by the decrease of the weight of the prostate gland of gonadectomized hamster treated with T plus finasteride or the new steroids. The IC50 value of these steroids was determined by measuring the conversion of radio labeled T to DHT. The results of this study carried out with 5alpha-reductase enzyme from hamster and human prostate showed that four of the six steroidal derivatives (5, 7, 9, 10) exhibited much higher 5alpha-reductase inhibitory activity, as indicated by the IC50 values than the presently used Proscar 3 (finasteride). The comparison of the weight of the hamster's prostate gland indicated that compound 5 had a comparable weight decrease as finasteride. The overall data of this study showed very clearly those compounds 5, 7, 9, 10 are good inhibitors for the 5alpha-reductase enzyme.

Published 14 March 2005 in Steroids, 70(3): 217-24.
Full-text of this article is available online (may require subscription).

© 2004-2008 Propecia Research Today. All Rights Reserved.